BMS-564929

• CAT Number: I004364
• CAS Number: 627530-84-1
• Molecular Formula: C14H12ClN3O3
• Molecular Weight: 305.72
• Purity: ≥95%
• Synonyms: 4-[(7R,7aS)-7-hydroxy-1,3-dioxo-5,6,7,7a-tetrahydropyrrolo[1,2-c]imidazol-2-yl]-2-chloro-3-methylbenzonitrile
• Target: Androgen Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• IC50: 2.11 ± 0.16 nM (Ki value)[1]

BMS-564929 is a novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (Ki= 2.11 nM).IC50 Value: 2.11 ± 0.16 nM (Ki value)[1]Target: Androgen receptorBMS-564929 has been advanced to clinical trials for the treatment of age-related functional decline. BMS-564929 is a subnanomolar AR agonist in vitro, is highly selective for the AR vs. other steroid hormone receptors, and exhibits no significant interactions with SHBG or aromatase.in vitro: BMS-564929 is a high affinity ligand for AR with a Ki of 2.11 ± 0.16 nM. This compound is more than 1000-fold selective for AR vs. ERα and β, GR, and MR, and approximately 400-fold selective vs. PR . BMS-564929 exhibited a potency (EC50, calculated as the concentration at which 50% of the maximum stimulatory effect of DHT is achieved) of 0.44 ± 0.03 nM compared with 2.81 ± 0.48 nM measured for T in the C2C12 myoblast cell line [1]. Sample preparation based on solid-phase extraction and subsequent LC-MS/MS measurement allowed for detection limits of 1-20 ng/mL, intra- and interday precisions of between 2.4 and 13.2% and between 6.5 and 24.2%, respectively [2].in vivo: The compound was administered across a wide dose range (1 μg to 1 mg/kg) for 8 wk in the same recovery schedule of administration as the 2-wk experiments. A dose-dependent increase in levator ani muscle and prostate wet weight was observed with BMS-564929 treatment, with ED50 values of 0.001 and 0.09 mg/kg for the levator ani and prostate, respectively [1]

Reference

[1]. Ostrowski J, Kuhns JE, Lupisella JA, Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats. Endocrinology. 2007 Jan;148(1):4-12.
[2]. Thevis M, Kohler M, Thomas A, Determination of benzimidazole- and bicyclic hydantoin-derived selective androgen receptor antagonists and agonists in human urine using LC-MS/MS. Anal Bioanal Chem. 2008 May;391(1):251-61.